Anti-cancerous efficacy and pharmacokinetics of 6-mercaptopurine loaded chitosan nanoparticles

Kumar GP 1 , Sanganal JS 2 , Phani AR 3 , Manohara C 2 , Tripathi SM 4 , Raghavendra HL 5 Show all authors , Janardhana PB 6 , Amaresha S 2 , Swamy KB 2 , Prasad RG 7

Affiliations 

  • 1 Department of Toxicology, Bioneeds India Private Limited, Bangalore, Karnataka, India; Department of Veterinary Pharmacology and Toxicology, Veterinary College, Bangalore, Karnataka, India. Electronic address: [email protected]
  • 2 Department of Veterinary Pharmacology and Toxicology, Veterinary College, Bangalore, Karnataka, India
  • 3 Nano Research for Advanced Materials and Technologies, Bangalore, Karnataka, India
  • 4 College of Veterinary Science and Animal Husbandry, Anjora, Durg, Chhattisgarh, India
  • 5 School of Medicine, College of Medical and Health Sciences, Wollega University, P.O. Box: 395, Nekemte, Ethiopia
  • 6 Stellixir Biotech Private Limited, T. Dasarahalli, Bangalore, Karnataka, India
  • 7 Faculty of Pharmaceutical Sciences, Asian Metropolitan University, Selangor, Kualalumpur, Malaysia
Pharmacol Res, 2015 Oct;100:47-57.
PMID: 26232590 DOI: 10.1016/j.phrs.2015.07.025

Abstract

6-Mercaptopurine is a cytotoxic and immunosuppressant drug. The use of this drug is limited due to its poor bioavailability and short plasma half-life. In order to nullify these drawbacks, 6-mercaptopurine-chitosan nanoparticles (6-MP-CNPs) were prepared and evaluated to study the influence of preparation conditions on the physicochemical properties by using DLS, SEM, XRD and FTIR. The in vitro drug release profile at pH 4.8 and 7.4 revealed sustained release patterns for a period of 2 days. The nanoformulations showed enhanced in vitro anti-cancer activities (MTT assay, apoptosis assay, cell cycle arrest and ROS indices) on HT-1080 and MCF-7 cells. In vivo pharmacokinetics profiles of 6-MP-CNPs showed improved bioavailability. Thus, the results of the present study revealed that, the prepared 6-MP-CNPs have a significant role in increasing anti-cancer efficacy, bioavailability and in vivo pharmacokinetics profiles.

* Title and MeSH Headings from MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine.

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